发明申请
- 专利标题： Cyclopropane compounds and pharmaceutical use thereof
- 专利标题（中）： 环丙烷化合物及其药物用途
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申请号： US12149683申请日： 2008-05-06
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公开(公告)号： US20080306258A1公开(公告)日： 2008-12-11
- 发明人: Takashi Inaba , Julia Haas , Makoto Shiozaki , Nicole M. Littmann , Katsutaka Yasue , Steven W. Andrews , Atushi Sakai , Andrew M. Fryer , Takafumi Matsuo , Ellen R. Laird , Akira Suma , Yuichi Shinozaki , Yoshikazu Hori , Hiroto Imai , Tamotsu Negoro
- 申请人： Takashi Inaba , Julia Haas , Makoto Shiozaki , Nicole M. Littmann , Katsutaka Yasue , Steven W. Andrews , Atushi Sakai , Andrew M. Fryer , Takafumi Matsuo , Ellen R. Laird , Akira Suma , Yuichi Shinozaki , Yoshikazu Hori , Hiroto Imai , Tamotsu Negoro
- 专利权人： Japan Tobacco Inc.
- 当前专利权人： Japan Tobacco Inc.
- 主分类号： C07D243/08
- IPC分类号： C07D243/08 ; C07D413/14
摘要：
The present invention provides a compound having aggrecanase inhibitory activity and MMP-13 inhibitory activity, and useful as a therapeutic agent for osteoarthritis, rheumatoid arthritis and the like, more specifically, a cyclopropane compound of formula (1): wherein R1 is —(CH2)m—X—(CH2)n-A1 etc., wherein m and n are the same or different and each is 0 to 6, X is a single bond, etc. and A1 is a substituted C3-14 hydrocarbon ring group, etc.; R2 and R3 are the same or different and each is a hydrogen atom, —(CH2)p—X1—(CH2)q-A2, etc., wherein p and q are the same or different and each is 0 to 6, X1 is a single bond, etc. and A2 is an optionally substituted C3-14 hydrocarbon ring group, etc.; R4 is —CO2R9, etc., wherein R9 is a hydrogen atom, etc.; and R20 and R21 are the same or different and each is a hydrogen atom, —(CH2)m12—X12—(CH2)m12—R30 etc., wherein m12 and m12 are the same or different and each is 0 to 6, X12 is a single bond, etc. and R30 is a hydrogen atom, etc.; or a prodrug thereof or a pharmaceutically acceptable salt thereof.
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